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Drugs used in cardio vascular system- Mr. panneh
1. DRUGS USED IN THE
CARDIO-VASCULAR
SYSTEM
MR. ABDOU
MARAM PANNEH
(RM
,FWACN,NT,
RN)
2. INTRODUCTION
Cardio vascular drugs are very diverse and can therefore be broadly
classified according to their pharmacological action.
These are:-
1. Angiotensin Converting Enzyme inhibitors (ACE).
2. Adrenergic Neuron Blockers
3. Alpha Blockers
4. Angiotensin II receptor Antagonists
5. Beta Blockers
6. Calcium Channel Blockers
7. Diuretics
8. Nitrates
9. Lipid Regulating Agents
10. Cardiac Glycosides
11. Centrally Acting Agents
12. Anticoagulants
13. Antiplatelets
3. 1. ANGIOTENSIN CONVERTING ENZYME
(ACE) INHIBITORS
GENERAL CHARACTERISTICS:-
ACE inhibitors block the conversion of angiotensin l to
angiotensin ll.
Angiotensin ll is a vasoconstrictor and promotes release of
aldosterone, causing salt and water retention, K+ loss and
reduces peripheral resistance.
ACE inhibitors thus lower blood pressure by vasodilatation
and promote loss of salt and water, thereby, elevate serum
K+.
They produce both preload and after load in patients with
heart failure.
CLINICAL USES:- Hypertension, Heart Failure and
Myocardial Infarction
6. 2. ANGIOTENSIN II RECEPTOR
ANTAGONISTS:
GENERAL CHARACTERISTICS:-
These drugs compete with angiotensin II for tissue
binding sites. They mainly act by selective blockage of
angiotensin I thus, reducing the pressure effects of
angiotensin II.
CLINICAL USES:- Treatment of hypertension.
ADR:- Nausea, diarrhea, abdominal pain, dizziness,
cough renal dysfunction, insomnia, sinusitis,
CONTRA-INDICATION:- Pregnancy & breastfeeding
(may cause malformation)
8. 3. ADRENERGIC NEURON
BLOCKERS:-
GENERAL CHARACTERISTICS
These drugs act by selectively inhibiting the transmission
in the adrenergic nerve endings.
CLINICAL USES:-
They have been used in hypertension but are now
superceeded by other antihypertensives.
Open-angle glaucoma treatment due to hypertension.
ADR:- nausea, diarrhea, dizziness, muscle weakness, etc
INTERACTION:- Anti histamines inhibit their effectiveness.
CONTRA INDICATIONS:- Avoid in pregnancy.
10. 3. ALPHA ADRENERGIC BLOCKERS / ALPHA
ADRENERGIC RECEPTOR ANTAGONISTS:
These drugs do block the effect of alpha1. Blockage of alpha1
adrenoreceptors inhibits vaso constriction caused by the
endogenous catecholamines (hormones, histamines).
This causes both arteriolar and venous vasodilation resulting in
a fall in blood pressure due to decrease peripheral resistance.
CLINICAL USES:- Hypertension, urinary obstruction in Benign
prostate hyperplasia.
ADR:- headache, dizziness, palpitations, priapism.
INTERACTION:- Diclofenac & Warfarin (hastens the excretion
of alpha blockers)
PRECAUTION:- avoid in pregnancy & breast feeding. Use in
men preferably.
12. 5. BETA ADRENERGIC BLOCKERS
These drugs are competitive antagonists at beta-
adrenergic receptor sites.
They reduce cardiac contractibility, thereby reducing
arterial pressure pulses.
They interrupt the renin-angiotensin-aldosterone
system, and decrease renin release from the kidneys.
Beta Blockers also block sympathetic stimulation at the
sinus node, which decreases the heart rate and cardiac
output, thereby lowering the blood pressure.
13. 5. BETA ADRENERGIC BLOCKERS Cont’d….
CLINICAL USES BETA ADRENERGIC BLOCKERS:-
Treatment of Hypertension & is often combined with diuretics
or other Antihypertensives.
Angina pectoris, Cardiac arrhythmias, myocardial infarction,
Heart Failure.
Control of sympathetic over activity in alcohol withdrawal,
anxiety states, hyperthyroidism, etc.
As eye drop in raised intra-ocular pressure of Glaucoma & ocular
hypertension.
ADR OF BETA ADRENERGIC BLOCKERS:- Depression,
sinusitis, Bradycardia, nervousness, fatigue, impotence,
headache, dizziness, nightmares, mood changes, nausea.
INTERACTION:- Insulin, Hydralazine, Prostaglandins
(interfere with the action of B/blockers)
15. 6. CALCIUM CHANNEL BLOCKERS / CALCIUM
ANTAGONISTS
These drugs inhibit cellular influx of calcium, which is
responsible for maintenance of the plateau phase of
the action potentials.
These affects the tissues that depend on calcium for
action.
Calcium Channel Blockers dilate coronary, peripheral
arteries and arterioles with little effect on venous tone.
CLINICAL USES:- Treatment & control of
hypertension, angina pectoris & cardiac arrhythmias.
ADR: same as beta blockers.
16. 6. CALCIUM CHANNEL BLOCKERS / CALCIUM
ANTAGONISTS Cont’d…
DRUGS USED:
Calcium Channel Blockers can be further classified into 3 major groups.
A. Benzothiazepines
- These group have less vasodilator activity.
- They have direct effect on the myocardium causing depression of SA & AV
nodal conduction.
- They are basically used in angina, hypertension and arrhythmia.
Examples:- Diltiazem (tildiem) 60mg
B. Phenylalkylamines
- They have similar effect as benzothiazepines
- They are widely used because of their anti arrhythmic, anti hypertensive &
anti anginal properties.
Examples: Verapamil (cordilox, securon) 40mg, 80mg, 120mg
17. CALCIUM CHANNEL BLOCKERS / CALCIUM
ANTAGONISTS Cont’d…
C. Dihydrophyridines
These of Calcium channel blockers have greater selectivity
on the vascular smooth muscles than for the myocardium.
Their main effect is on vaso dilation.
They also have both antihypertensive, anti arrhythmic and
anti anginal properties.
They are the ones that are more commonly used.
Examples:
Amlodipine (amlor, istin) 5mg, 10mg, 20mg
Nifedipine (adalat, nifelat) 2.5mg, 5mg, 10mg, 20mg, 30mg
Felodipine (plendil) 2,5mg, 5mg, 10mg
Nisoldipine (syscor) 10mg, 20mg, 30mg
Nicardipine (cardene)20mg, 30mg
18. 7. DIURETICS
GENERAL CHARACTERISTICS:-
They lower B/P by depleting the volume of sodium and
blood volume.
Some have vasodilator effects.
Others can block the transport function of the renal
tubules and prevent water reabsorption.
There are several types of diuretics. These are:-
Loop Diuretics
Thiazides Diuretics
Carbonic Anhydrase inhibitors Diuretics
Potassium Sparing Diuretics Others:- osmotic
diuretics
- Anti diuretic hormone antagonists.
19. 7. DIURETICS Cont’d….
A. Loop Diuretics
These products selectively inhibit the reabsorption of sodium chloride in the Loop
of Henle.
They are the most powerful and efficacious diuretics.
They are usually employed in hypertensive crises.
CLINICAL USES:
Pulmonary edema with congestive heart failure
Edema that does not respond to less powerful diuretics and is caused by hepatic,
renal or cardiac conditions
Hypertension that cannot be controlled with other types of diuretics
ADR - ototoxicity, allergic reactions, GIT disorders(nausea, vomiting,etc),
dehydration, hypokalemia, hypocalcemia, hypotension, hyperglycemia,
photosensitivity.
PRECAUTION: allergy to sulphonamides, anuria, hypovolemia, B/feeding, infants.
INTERACTIONS:-
Digtalis:- increase risk of digitalis toxicity
NSAIDs:- inhibits the effect of loop diuretics
Lithium:- reduces the excretion of lithium.
21. 7. DIURETICS Cont’d…
Thiazides Diuretics
These drugs are chemically related to the sulfonamides and
similar effects to the loop diuretics.
They products block the transport function of renal tubules and
also inhibit water re-absorption
They are well absorbed when given orally and are excreted
through the kidneys via urine.
CLINICAL USES:- treatment of essential Hypertension, Fluid
retention due to heart failure, hepatic or renal disease.
ADR:
impotence due to loss of electrolytes
Dehydration, photosensitivity, paresthesias, hyperglycemia, etc..
23. 7. DIURETICS Cont’d…
C. Potassium Sparing Diuretics
These products inhibits the elimination of potassium form the
renal tubules.
CLINICAL USE:- Treat hypertension and edema. Prevent
hypokalemia
ADR:- Gynaecomastia, menstrual irregularities, erectile
dysfunction, deepening of voice, leg cramps, dizziness, acute
renal failure, kidney stones
INTERACTION: ACE inhibitors, potassium supplements,
Indomethacin- can all cause increase risk of hyperkalemia.
Aspirin – blocks the effects of diuretics.
Examples of Drugs Used:-
Spironolactone (aldactone) 25mg, 50mg, 100mg tabs
Amiloride(midamor) 5mg tabs
Triamterene (dytac, dyrenium) 50mg caps
24. 7. DIURETICS Cont’d…
D. Osmotic Diuretics
These products raised the osmolality of plasma and renal
tubules fluid.
They maintain urine output and prevent renal failure as in
hypovolemic shock.
They reduce intracranial pressure caused by cerebral
oedema.
Reduces intraocular pressure by drawing fluid from the
eyes.
Eliminates toxins through the kidneys.
ADR: Edema, fluid & electrolyte imbalance, nausea &
vomiting, headache, rebound ICP.
PRECAUTION:_ in renal failure
Examples:
Mannitol 5%, 10%, 15%, 20%, etc infusion.
25. 7. DIURETICS Cont’d…
E. Carbonic Anhydrate Inhibitors Diuretics
These are weak diuretics and are used mainly to reduce
raised intra-ocular pressure.
CLINICAL USES: open-angle glaucoma, epilepsy, acute
mountain sickness.
ADR: fatigue, drowsiness, depression, excitement,
hypokalemia, paraesthesia. Aplastic anemia, rash, pruritis,
tinnitus, etc
INTERACTION: Aspirin – may cause acidosis.
Examples:-
Brinzolamide
Diclofenamide
Dorzolamide
Methazolamide.
26. 8. NITRATES
These drugs are peripheral and coronary vasodilators.
They relax smooth muscles in the blood vessel walls, and thus,
help reduce pain of anginal attacks..
They redistribute blood flow to ischemic areas of the
myocardium, which improves perfusion of the heart.
They dilate the veins, reducing venous pressure and venous
return.
They reduce blood volume and pressure within the heart,
thereby reducing preload-which is the distending force that
stretches the ventricular muscle prior to electrical excitation and
contraction of the heart muscles.
They dilate arterioles, which lowers peripheral vascular
resistance.
CLINICAL USES:- Acute, Stable & unstable angina, acute &
chronic heart failure.
ADR:- dizziness, hypotension, weakness, nausea & vomiting,
pulsating headache.
27. 8. NITRATES Cont’d…
PRECAUTION:- avoid IV administration to clients
with hypovolemia or severe hypertension.
Administer with caution to clients with carotid
disease, constrictive pericarditis, cardiac tamponade,
severe hypertension.
Examples of Drugs used:
NGT/Nitroglycerin (Nitro-Bid, Nitrostat, Nitrodisc,
Nitrogard) tabs (oral / sublingually)
Glycerin trinitrate- sublingual tabs 300mcg, 600mcg
Isosorbide dinitrate(isordil, isocard) 5mg, 10mg tabs
Isosorbide Mononitrate(isotrate, ismo, monit) 10mg,
20mg, 40mg tabs
28. 9. LIPID REGULATING AGENTS
These drugs are used to modify blood lipid
concentration in the management of hyperlipidaemia.
They are also used in the reduction of cardiovascular
arrest.
These drugs are grouped into five:-
A- The Statins
B- The Fibrates
C- Bile-acid binding resins
D- Nicotinates
E- Omega-3 Triglycerides
29. 9. LIPID REGULATING AGENTS
Cont’d…
A. The Statins
These drugs help to reduce cholesterol by stimulating an
increase in the Low Density Lipoproteins (LDL), or
hapocytes memnrane, causing an increase clearance in
LDL from the circulation.
This reduces LDL cholesterol and some triglyceride.
CLINICAL USES:- Coronary artery bypass, cerebrovascular
disease, peripheral vascular disease, high total serum-
cholesterol level, etc
ADR:- Headache, altered liver function tests, abdominal
Pain, flatulence, nausea & vomiting, rash.
CONTRA_INDICATION:- Pregnancy, active liver disease.
31. 9. LIPID REGULATING AGENTS Cont’d…
B. The Fibrates
These are derivatives of fibric acid.
They inhibit the synthesis of cholesteroland bile acids thereby
enhancing their secretion.
They are broad spectrum lipid regulating agents. Their main
action is to decrease serum triglycerides and LDL cholesterol
level and to raise the High Density Lipoproteins (HDL)-
cholesterol level.
USES:- To treat clients with hyperlipideamia who fail to respond
to treatment or at risk of pancreatitis.
ADR:- Abdominal pains, headache, eczema, fatigue, liver tumors
Examples:-
Bezafibrate (Bzalip) 200mg tabs
Ciprofibrate (modalim) 100mg tabs
Fenafibrate (lipantil) 67mg, 200mg 267mg caps
32. 9. LIPID REGULATING AGENTS
Cont’d…
C. Bile-Acid Binding Resins
These products lower cholesterol by combining with
bile acids in the GIT and preventing their
reabsorption.
They increase the oxidation of cholesterol to replace
bile acids loss.
USES:- Treatment of hypercholesterolemia in adults.
ADR:- constipation, pruritis, headache, nausea,
bloating and flatulence.
Examples:
colestipol (colestid)
Cholestyramine (questran, prevalite powder)
Colesevelam, Divistyramine.
33. 9. LIPID REGULATING AGENTS
Cont’d…
D. Nicotines
These drugs reduce triglycerides level and increase the
LDL cholesterol.
They are mainly used in hypertriglyceridaemia.
Examples:-
Niceritrol
Acipimox (olbetam) 520mg
Sorbinicate
Nicotinic acid 50mg
34. 9. LIPID REGULATING AGENTS
Cont’d…
E. Omega-3 Triglycerides
These are long chain polyunsaturated fatty acids that
primarily reduce triglycerides.
They reduce plasma triglycerides in clients with severe
hypertriglyceridaemia with risk of ischemic heart
disease.
ADR: occasional nausea and belching.
Examples:-
Omega-3 Fish oil.
35. 10. CARDIAC GLYCOSIDES.
These products increase cardiac output especially when the
heart is failing.
They inhibit sodium-potassium adenosine trphosphate.
They also reduce conductivity in the heart, especially
through the atrio-ventricular node and therefore, have a
negative chronotropic effect.
They are used to slow the heart rate in supraventricular
arrhythmias in heart failure.
ADR:- nausea & vomiting, fatigue, drowsiness, confusion,
arrhythmias,gynaecomastia.
Examples:-
Digoxin (lanoxin) 62.5cmg, 125mcg, 250mcg
Digitalis lanata, Digitalis Leaf, Digitoxin,etc.
36. 11. CENTRALLY ACTING AGENTS:
These products act like alpha2 adreno-receptor antagonists.
They act by stimulating alpha2 adrenocptors in the CNS causing
a reduction in sympathetic tone and a resultant fall in blood
pressure.They also reduce the heart rate.
However, they have been superceeded by other antihypertensive
drugs because of their adverse effects.
ADR:- dry mouth, paraesthesia, stomatitis, Bradycardia,
depression, nightmares, impotence, gynaecomastia, mild
psychosis, decreased libido.
Examples:
Methyldopa (aldomet) 125mg,250mg, 500mg
Moxonidine (physiotens) 200mcg, tabs
Clonidine, Brimonidine, Triamenidine, Guanfacine, Apraclonidine.
37. 12. ANTICOAGULANTS:-
These products are used in the treatment and
prophylaxis of thromboembolic disorders.
ADR:- bleeding, local pain at injection site,
Osteoporosis, alopecia
INTERACTION:- Tetracyclines, Nicotine, Digitalis
glycosides – these drug decreases the effect of
anticoagulants.
They can be divided into two types:-
Direct anticoagulants
Indirect anticoagulants.
38. 12. ANTICOAGULANTS Cont’d:-
A. Direct Anti coagulants
These group of anti coagulants act by inhibiting the cloting of blood
in vitro and in vivo by enhancing the action of antithrombin III.
Antithrombin III is present in plasma and inhibit the activity of
activated clotting factors.
CLINICAL USES:- Prophylaxis and treatment of thromboembolic
disorders, maintains patency of IV catheters, Useful DIC,
Prevention of blood clotting in cardiac and vascular surgery.
DRUGSVOMMONLY USED:-
Heparin1000Iu/ml, 5000Iu/ml, 25000Iu/ml injection
Cetoparin (alphaparin)3000IU injection
Dalteparin 12500UI/ml injection
Reviparin (clivarin) 1432IU/0.25ml
Tinzaparin 10000IU/ml
Danaparoid sodium (orgaran) 1250IU/ml injection
39. 12. ANTICOAGULANTS Cont’d:-
B. Indirect Anti-coagulants:-
The products act by depressing the hepatic vitamin K-
dependant synthesis of coagulation factors II
(prothrombin), VII, IX and X.
They also suppress the anticoagulant protein C and its
co-factor proteins.
DRUGS USED:
Warfarin 0.5mg, 1mg, 3mg, 5mg tabs
Acenocoumarol (sinthrome) 1mg tabs
Phenindione (Dindevan) 10mg, 25mg, 50mg tabs
40. 13. ANTI-PLATELET AGENTS
Platelet aggregation is very important in homeostatis.
It is also involved in thrombos formation especially in
arterial circulation.
Antiplatelet drugs reduce platelet aggregation and are used
to prevent thromembolic events in patients who have
suffered myocardial infarction, ischemic stroke or transient
ischemic attack or unstable angina.
They are also used for primary prevention of
thromboembolic events in patients at risk,
Antiplatelet drugs act by inhibiting platelet cyclo-
oxygenase and thus preventing synthesis of thromboxanes
A2.
ADR:- bleeding manifestation, hypotension, Bradycardia,
headache, fever, chest pain,
CONTRA-INDICATION: pregnancy, breastfeeding.